JP2011246469A5 - - Google Patents
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- Publication number
- JP2011246469A5 JP2011246469A5 JP2011138647A JP2011138647A JP2011246469A5 JP 2011246469 A5 JP2011246469 A5 JP 2011246469A5 JP 2011138647 A JP2011138647 A JP 2011138647A JP 2011138647 A JP2011138647 A JP 2011138647A JP 2011246469 A5 JP2011246469 A5 JP 2011246469A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- pivaloyl
- mesylate
- benzoyl
- hydrogen succinate
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- LULAYUGMBFYYEX-UHFFFAOYSA-N 3-chlorobenzoic acid Chemical compound OC(=O)C1=CC=CC(Cl)=C1 LULAYUGMBFYYEX-UHFFFAOYSA-N 0.000 claims 78
- 125000000217 alkyl group Chemical group 0.000 claims 62
- YQTCQNIPQMJNTI-UHFFFAOYSA-N 2,2-dimethylpropan-1-one Chemical group CC(C)(C)[C]=O YQTCQNIPQMJNTI-UHFFFAOYSA-N 0.000 claims 41
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 41
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 41
- KDYFGRWQOYBRFD-UHFFFAOYSA-M succinate(1-) Chemical compound OC(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-M 0.000 claims 41
- 150000001875 compounds Chemical class 0.000 claims 25
- 239000000203 mixture Substances 0.000 claims 25
- 239000001177 diphosphate Substances 0.000 claims 20
- XPPKVPWEQAFLFU-UHFFFAOYSA-J diphosphate(4-) Chemical compound [O-]P([O-])(=O)OP([O-])([O-])=O XPPKVPWEQAFLFU-UHFFFAOYSA-J 0.000 claims 20
- 235000011180 diphosphates Nutrition 0.000 claims 20
- 150000004712 monophosphates Chemical class 0.000 claims 20
- 239000001226 triphosphate Substances 0.000 claims 20
- 235000011178 triphosphate Nutrition 0.000 claims 20
- 125000002264 triphosphate group Chemical group [H]OP(=O)(O[H])OP(=O)(O[H])OP(=O)(O[H])O* 0.000 claims 14
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 229960004413 flucytosine Drugs 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- UNXRWKVEANCORM-UHFFFAOYSA-N triphosphoric acid Chemical compound OP(O)(=O)OP(O)(=O)OP(O)(O)=O UNXRWKVEANCORM-UHFFFAOYSA-N 0.000 claims 6
- 208000002672 hepatitis B Diseases 0.000 claims 4
- 241001465754 Metazoa Species 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- IKCLCGXPQILATA-UHFFFAOYSA-N 2-chlorobenzoic acid Chemical compound OC(=O)C1=CC=CC=C1Cl IKCLCGXPQILATA-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10711698P | 1998-11-05 | 1998-11-05 | |
| US60/107,116 | 1998-11-05 | ||
| US11565399P | 1999-01-13 | 1999-01-13 | |
| US60/115,653 | 1999-01-13 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000579613A Division JP2002528554A (ja) | 1998-11-05 | 1999-11-05 | Ｂ型肝炎ウイルス活性を持ったヌクレオシド |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011246469A JP2011246469A (ja) | 2011-12-08 |
| JP2011246469A5 true JP2011246469A5 (OSRAM) | 2012-09-06 |
Family
ID=26804401
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000579613A Withdrawn JP2002528554A (ja) | 1998-11-05 | 1999-11-05 | Ｂ型肝炎ウイルス活性を持ったヌクレオシド |
| JP2011138647A Pending JP2011246469A (ja) | 1998-11-05 | 2011-06-22 | Ｂ型肝炎ウイルス活性を持ったヌクレオシド |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000579613A Withdrawn JP2002528554A (ja) | 1998-11-05 | 1999-11-05 | Ｂ型肝炎ウイルス活性を持ったヌクレオシド |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US6458773B1 (OSRAM) |
| EP (1) | EP1124839B1 (OSRAM) |
| JP (2) | JP2002528554A (OSRAM) |
| KR (1) | KR100618028B1 (OSRAM) |
| CN (1) | CN1216893C (OSRAM) |
| AT (1) | ATE315574T1 (OSRAM) |
| AU (1) | AU774720B2 (OSRAM) |
| BR (1) | BR9915555A (OSRAM) |
| CA (1) | CA2348470C (OSRAM) |
| DE (1) | DE69929460D1 (OSRAM) |
| IL (2) | IL142983A0 (OSRAM) |
| MX (1) | MXPA01004504A (OSRAM) |
| WO (1) | WO2000026225A2 (OSRAM) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL138037A0 (en) * | 1998-02-25 | 2001-10-31 | Univ Emory | 2'-fluoronucleosides |
| MY164523A (en) | 2000-05-23 | 2017-12-29 | Univ Degli Studi Cagliari | Methods and compositions for treating hepatitis c virus |
| CZ301182B6 (cs) * | 2000-05-26 | 2009-12-02 | Idenix (Cayman) Limited | Použití nukleosidových derivátu pro výrobu farmaceutických prostredku pro lécení infekcí vyvolaných flaviviry a pestiviry |
| US7589077B2 (en) | 2001-05-18 | 2009-09-15 | Rakesh Kumar | Antiviral nucleosides |
| US7608600B2 (en) * | 2002-06-28 | 2009-10-27 | Idenix Pharmaceuticals, Inc. | Modified 2′ and 3′-nucleoside prodrugs for treating Flaviviridae infections |
| CN101172993A (zh) | 2002-06-28 | 2008-05-07 | 埃迪尼克斯(开曼)有限公司 | 用于治疗黄病毒感染的2′－c－甲基－3′－o－l－缬氨酸酯核糖呋喃基胞苷 |
| WO2004002422A2 (en) | 2002-06-28 | 2004-01-08 | Idenix (Cayman) Limited | 2’-c-methyl-3’-o-l-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections |
| US20040067877A1 (en) | 2002-08-01 | 2004-04-08 | Schinazi Raymond F. | 2', 3'-Dideoxynucleoside analogues for the treatment or prevention of Flaviviridae infections |
| DE60329211D1 (de) * | 2002-10-31 | 2009-10-22 | Metabasis Therapeutics Inc | Cytarabin-monophosphate prodrugs |
| ES2624353T3 (es) | 2002-11-15 | 2017-07-13 | Idenix Pharmaceuticals Llc | 2'-Metil nucleósidos en combinación con interferón y mutación de Flaviviridae |
| RU2005121904A (ru) | 2002-12-12 | 2006-01-20 | Айденикс (Кайман) Лимитед (Ky) | Способ получения 2`-разветвленных нуклеозидов |
| JP5254033B2 (ja) | 2005-12-23 | 2013-08-07 | イデニク プハルマセウティカルス，インコーポレイテッド | 分岐型ヌクレオシドを調製するための合成中間体の製造方法 |
| WO2015123352A1 (en) | 2014-02-13 | 2015-08-20 | Ligand Pharmaceuticals, Inc. | Prodrug compounds and their uses |
| US9994600B2 (en) | 2014-07-02 | 2018-06-12 | Ligand Pharmaceuticals, Inc. | Prodrug compounds and uses therof |
| AU2019207625A1 (en) | 2018-01-09 | 2020-07-30 | Ligand Pharmaceuticals, Inc. | Acetal compounds and therapeutic uses thereof |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4681933A (en) | 1986-05-01 | 1987-07-21 | University Of Georgia Research Foundation, Inc. | 2',3'-dideoxy-5-substituted uridines and related compounds as antiviral agents |
| US5084445A (en) | 1986-05-01 | 1992-01-28 | University Of Georgia Research Foundation, Inc. | 3'-azido-2',3'-dideoxy-5-methylcytidine |
| US4916122A (en) | 1987-01-28 | 1990-04-10 | University Of Georgia Research Foundation, Inc. | 3'-Azido-2',3'-dideoxyuridine anti-retroviral composition |
| US5077279A (en) | 1986-05-01 | 1991-12-31 | University Of Georgia Research Foundation, Inc. | 3'-azido-2',3'-dideoxy-5-methylcytidine anti-viral composition |
| US4841039A (en) | 1986-05-01 | 1989-06-20 | Emory University | 2',3'-dideoxy-5-substituted uridines and related compounds as antiviral agents |
| US5190926A (en) | 1987-01-28 | 1993-03-02 | University Of Georgia Research Foundation, Inc. | 3'-azido-2',3'-dideoxypyrimidines and related compounds as antiviral agents |
| US5047407A (en) | 1989-02-08 | 1991-09-10 | Iaf Biochem International, Inc. | 2-substituted-5-substituted-1,3-oxathiolanes with antiviral properties |
| US5041449A (en) | 1988-04-11 | 1991-08-20 | Iaf Biochem International, Inc. | 4-(nucleoside base)-substituted-1,3-dioxolanes useful for treatment of retroviral infections |
| NZ228645A (en) | 1988-04-11 | 1991-09-25 | Iaf Biochem Int | 1,3-dioxolane derivatives substituted in the 5th position by a purine or pyrimidine radical; treatment of viral infections |
| DD293498A5 (de) * | 1989-07-20 | 1991-09-05 | Zi Fuer Molekularbiologie Der Adw,De | Verfahren zur herstellung eines mittels fuer die behandlung oder prophylaxe von hepatits-infektionen bei mensch und tier |
| US5204466A (en) | 1990-02-01 | 1993-04-20 | Emory University | Method and compositions for the synthesis of bch-189 and related compounds |
| DE4224737A1 (de) * | 1992-07-27 | 1994-02-03 | Herbert Prof Dr Schott | Neue Cytosinnucleosidanaloga, Verfahren zu ihrer Herstellung und ihre Verwendung |
| FR2709754B1 (fr) | 1993-09-10 | 1995-12-01 | Centre Nat Rech Scient | Composés 2' ou 3'-déoxy- et 2', 3'-didéoxy-beta-L-pentofuranonucléosides, procédé de préparation et application thérapeutique, notamment anti-virale. |
| CA2171550C (en) * | 1993-09-10 | 2008-08-26 | Raymond F. Schinazi | Nucleosides with anti-hepatitis b virus activity |
| DE4418690A1 (de) | 1994-05-28 | 1996-01-11 | Boehringer Mannheim Gmbh | Neue Lipidester von Nucleosid-Monophosphaten und deren Verwendung als immunsuppressive Arzneimittel |
| US5559101A (en) | 1994-10-24 | 1996-09-24 | Genencor International, Inc. | L-ribofuranosyl nucleosides |
| US5703058A (en) | 1995-01-27 | 1997-12-30 | Emory University | Compositions containing 5-fluoro-2',3'-didehydro-2',3'-dideoxycytidine or a mono-, di-, or triphosphate thereof and a second antiviral agent |
| ATE346651T1 (de) | 1995-06-07 | 2006-12-15 | Univ Emory | Nucleoside mit anti-hepatitis b virus wirksamkeit |
| WO1997009052A1 (en) | 1995-09-07 | 1997-03-13 | University Of Georgia Research Foundation, Inc. | Therapeutic azide compounds |
| JP2002503212A (ja) | 1996-10-16 | 2002-01-29 | アイ・シー・エヌ・フアーマシユーテイカルズ・インコーポレイテツド | 単環式ヌクレオシド、その類似体および使用 |
-
1999
- 1999-11-05 CA CA002348470A patent/CA2348470C/en not_active Expired - Fee Related
- 1999-11-05 AT AT99958793T patent/ATE315574T1/de not_active IP Right Cessation
- 1999-11-05 BR BR9915555-9A patent/BR9915555A/pt not_active IP Right Cessation
- 1999-11-05 AU AU16085/00A patent/AU774720B2/en not_active Ceased
- 1999-11-05 IL IL14298399A patent/IL142983A0/xx active IP Right Grant
- 1999-11-05 US US09/435,261 patent/US6458773B1/en not_active Expired - Lifetime
- 1999-11-05 CN CN998141895A patent/CN1216893C/zh not_active Expired - Fee Related
- 1999-11-05 MX MXPA01004504A patent/MXPA01004504A/es not_active IP Right Cessation
- 1999-11-05 KR KR1020017005679A patent/KR100618028B1/ko not_active Expired - Fee Related
- 1999-11-05 EP EP99958793A patent/EP1124839B1/en not_active Expired - Lifetime
- 1999-11-05 DE DE69929460T patent/DE69929460D1/de not_active Expired - Lifetime
- 1999-11-05 WO PCT/US1999/026157 patent/WO2000026225A2/en not_active Ceased
- 1999-11-05 JP JP2000579613A patent/JP2002528554A/ja not_active Withdrawn
-
2001
- 2001-05-04 IL IL142983A patent/IL142983A/en not_active IP Right Cessation
-
2011
- 2011-06-22 JP JP2011138647A patent/JP2011246469A/ja active Pending
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